EP3781575A4 - Makrocyclische kondensierte pyrazole als mcl-1-inhibitoren - Google Patents

Makrocyclische kondensierte pyrazole als mcl-1-inhibitoren Download PDF

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Publication number
EP3781575A4
EP3781575A4 EP20744299.7A EP20744299A EP3781575A4 EP 3781575 A4 EP3781575 A4 EP 3781575A4 EP 20744299 A EP20744299 A EP 20744299A EP 3781575 A4 EP3781575 A4 EP 3781575A4
Authority
EP
European Patent Office
Prior art keywords
pyrrazoles
mcl
macrocyclic
inhibitors
fused
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
EP20744299.7A
Other languages
English (en)
French (fr)
Other versions
EP3781575A1 (de
Inventor
Guozhi Tang
Dongbo Li
Liugen LI
Xianchan ZHA
Wenming CHEN
Shaomeng Wang
Chao-Yie Yang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Ascentage Pharma Suzhou Co Ltd
Ascentage Pharma Group Co Ltd
University of Michigan
Original Assignee
Ascentage Pharma Suzhou Co Ltd
Ascentage Pharma Group Co Ltd
University of Michigan
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ascentage Pharma Suzhou Co Ltd, Ascentage Pharma Group Co Ltd, University of Michigan filed Critical Ascentage Pharma Suzhou Co Ltd
Publication of EP3781575A1 publication Critical patent/EP3781575A1/de
Publication of EP3781575A4 publication Critical patent/EP3781575A4/de
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D515/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D497/00Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D497/22Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
EP20744299.7A 2019-01-23 2020-01-22 Makrocyclische kondensierte pyrazole als mcl-1-inhibitoren Pending EP3781575A4 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2019072801 2019-01-23
PCT/CN2020/073742 WO2020151738A1 (en) 2019-01-23 2020-01-22 Macrocyclic fused pyrrazoles as mcl-1 inhibitors

Publications (2)

Publication Number Publication Date
EP3781575A1 EP3781575A1 (de) 2021-02-24
EP3781575A4 true EP3781575A4 (de) 2021-06-02

Family

ID=71735845

Family Applications (1)

Application Number Title Priority Date Filing Date
EP20744299.7A Pending EP3781575A4 (de) 2019-01-23 2020-01-22 Makrocyclische kondensierte pyrazole als mcl-1-inhibitoren

Country Status (5)

Country Link
US (1) US20220396587A1 (de)
EP (1) EP3781575A4 (de)
CN (1) CN112204036B (de)
TW (1) TWI760685B (de)
WO (1) WO2020151738A1 (de)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109715632B (zh) 2016-05-19 2021-10-26 拜尔公开股份有限公司 大环吲哚衍生物
WO2019096905A1 (en) 2017-11-17 2019-05-23 Bayer Aktiengesellschaft Macrocyclic chlorine substituted indole derivatives
EP3710449B1 (de) 2017-11-17 2022-07-06 The Broad Institute, Inc. Makrocyclische fluorsubstituierte indolderivate als mcl-1-inhibitoren zur verwendung bei der behandlung von krebs
TWI810220B (zh) 2017-11-17 2023-08-01 德商拜耳廠股份有限公司 經取代之巨環吲哚衍生物
TW201932473A (zh) 2017-11-17 2019-08-16 美商博德研究所有限公司 巨環吲哚衍生物
EP3710450A1 (de) 2017-11-17 2020-09-23 Bayer Aktiengesellschaft Makrocyclische chlorsubstituierte indolderivate
EP3924358A4 (de) * 2019-03-08 2023-07-05 Zeno Management, Inc. Makrocyclische verbindungen
WO2021099579A1 (en) 2019-11-21 2021-05-27 Janssen Pharmaceutica Nv Macrocyclic indole derivatives as mcl-1 inhibitors
CN114728986A (zh) 2019-11-21 2022-07-08 詹森药业有限公司 作为mcl-1抑制剂的大环磺酰基衍生物
KR20220143906A (ko) * 2020-02-21 2022-10-25 얀센 파마슈티카 엔.브이. Mcl-1의 억제제로서의 거대환식 인돌 유도체
CA3178283A1 (en) 2020-05-29 2021-12-02 Frederik Jan Rita Rombouts Macrocyclic 7-pyrazol-5-yl-indole derivatives as inhibitors of mcl-1
US20230234969A1 (en) 2020-06-19 2023-07-27 Janssen Pharmaceutica Nv N-linked macrocyclic 7-(pyrazol-5-yl)-indole derivatives as inhibiors of mcl-1
WO2022032284A1 (en) * 2020-08-07 2022-02-10 Zeno Management, Inc. Macrocyclic compounds
EP4236938A1 (de) * 2020-11-02 2023-09-06 Merck Sharp & Dohme LLC Makrocyclische harnstofforexinrezeptoragonisten
WO2022251247A1 (en) * 2021-05-28 2022-12-01 Zeno Management, Inc. Macrocyclic compounds
CN115490708A (zh) * 2021-06-18 2022-12-20 苏州亚盛药业有限公司 磺酰胺类大环衍生物及其制备方法和用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020185606A1 (en) * 2019-03-08 2020-09-17 Zeno Management, Inc. Macrocyclic compounds
WO2020221272A1 (zh) * 2019-04-30 2020-11-05 江苏恒瑞医药股份有限公司 吲哚类大环衍生物、其制备方法及其在医药上的应用

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2009011211A (es) * 2007-04-16 2009-10-30 Abbott Lab Indoles sustituidos en la posicion 7 inhibidores de mci-1.
US9949965B2 (en) * 2014-10-17 2018-04-24 Vanderbilt University Tricyclic indole Mcl-1 inhibitors and uses thereof
KR102388208B1 (ko) * 2016-04-22 2022-04-18 아스트라제네카 아베 암을 치료하기 위한 거대 환형 mcl1 억제제
JP6453507B2 (ja) * 2017-03-30 2019-01-16 アムジエン・インコーポレーテツド Mcl−1タンパク質を阻害する化合物
TW201904976A (zh) * 2017-03-31 2019-02-01 瑞典商阿斯特捷利康公司 Mcl-1抑制劑及其使用方法
TWI781996B (zh) * 2017-03-31 2022-11-01 瑞典商阿斯特捷利康公司 合成mcl-1抑制劑之方法

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020185606A1 (en) * 2019-03-08 2020-09-17 Zeno Management, Inc. Macrocyclic compounds
WO2020221272A1 (zh) * 2019-04-30 2020-11-05 江苏恒瑞医药股份有限公司 吲哚类大环衍生物、其制备方法及其在医药上的应用

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of WO2020151738A1 *

Also Published As

Publication number Publication date
WO2020151738A1 (en) 2020-07-30
TW202043241A (zh) 2020-12-01
EP3781575A1 (de) 2021-02-24
CN112204036A (zh) 2021-01-08
TWI760685B (zh) 2022-04-11
US20220396587A1 (en) 2022-12-15
CN112204036B (zh) 2022-12-27

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